In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes

  • Eur J Pharmacol. 1980 Mar 21;62(2-3):225-8. doi: 10.1016/0014-2999(80)90281-2.
P Placheta ,  M Karobath
PMID: 6103810 DOI: 10.1016/0014-2999(80)90281-2
Abstract

SQ 20009 and SQ 65396, two new pyrazolopyridines with anxiolytic properties in Animals, reversibly increased Na+-independent 3H-GABA binding to rat cerabral cortex membranes in vitro. This modulation was partially chloride dependent and sensitive to Triton-X 100. Kinetic analysis of 3H-muscimol binding revealed an increase of the apparent number of binding sites. The results are compatible with a functional association between Na+-independent GABA binding sites and the GABA/benzodiazepine receptor complex.

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